Bioassay-directed drug discovery efforts focusing on various species of the genus Hypericum led to the discovery of a number of new acylphloroglucinols including (S,E)-1-(2-((3,7-dimethylocta-2,6-dien-1-yl)oxy)-4,6-dihydroxyphenyl)-2-methylbutan-1-one (6, olympicin A) from H. olympicum, with MICs ranging from 0.5 to 1 mg/L against a series of clinical isolates of multi-drug-resistant (MDR) and methicillin-resistant Staphylococcus aureus (MRSA) strains. The promising activity and interesting chemistry of olympicin A prompted us to carry out the total synthesis of 6 and a series of analogues in order to assess their structure-activity profile as a new group of antibacterial agents. Following the synthesis of 6 and structurally-related acylphloroglucinols 7–15 and 18–24, their antibacterial activities against a panel of S. aureus strains were evaluated. The presence of an alkyloxy group consisting of 8–10 carbon atoms ortho to a five-carbon acyl substituent on the phloroglucinol core are important structural features for promising anti-staphylococcal activity.

以生物测定为导向的药物发现工作着眼于金丝桃属的各种物种，导致发现了许多新的酰基间苯三酚，包括（S，E）-1-（2-（（3,7-dimethylocta-2,6-dien-来自H的1-基）氧基）-4,6-二羟基苯基）-2-甲基丁-1--1-酮（6，奥比汀A）。olympicum，与MIC值范围为0.5至1mg / L与一系列多药耐药（MDR）和耐甲氧西林的临床分离株的金黄色葡萄球菌（MRSA）菌株。奥林匹克霉素A的有前途的活性和有趣的化学反应促使我们进行6的全合成以及一系列类似物，以评估它们作为一组新的抗菌剂的结构活性特征。以下的合成6和结构上相关的acylphloroglucinols 7 - 15和18 - 24，其对一组抗细菌活性的金黄色葡萄球菌菌株进行评价。在间苯三酚核心上，由一个8至10个碳原子邻位至一个5个碳原子的酰基取代基组成的烷氧基的存在是重要的结构特征，有望实现抗葡萄球菌的活性。